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K858 (Racemic) is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM. Eg5 is a key protein involved in the formation of bipolar spindles. K858 induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines.
Molecular Weight | 277.34 |
Formula | C13H15N3O2S |
CAS Number | 72926-24-0 |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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AZD4877
AZD4877 is another isostere to Ispinesiband also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. |
Filanesib TFA
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. |
Filanesib hydrochloride
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. |
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Eg5-IN-1 is a potent kinesin family motor protein (Eg5) inhibitor with an IC50 value of 1.97 µM. |
PVZB-1194
PVZB-1194 is a biphenyl-type inhibitor of kinesin Eg5 that induces apoptosis by inhibiting Eg5 ATPase activity and shows potent kinesin spindle protein (KSP) inhibition only in the presence of microtubules, with anticancer activity. |
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